1. Field of the Invention
The present invention relates to useful therapeutic quaternary ammonium salt forms of pilocarpine. More particularly, the present invention pertains to newly developed quaternary ammonium salt forms of pilocarpine which are characterized as being much more lipophilic in comparison to the parent moiety, pilocarpine, per se.
These newly developed quaternary ammonium salt forms of pilocarpine are extremely useful as antiglaucoma agents, and they can be administered topically to warm-blooded animals, e.g., humans, per se, or in any pharmaceutically acceptable ophthalmic composition form when admixed with a suitable pharmaceutically acceptable inert ophthalmic carrier.
2. Description of the Prior Art
A pharmaceutical and medical need exists for new and useful compounds indicated for the management of glaucoma in warm-blooded animals. This need exists because the compound of choice, pilocarpine, exhibits extremely poor lipoidal solubility which tends to restrict ophthalmic application of the drug in the treatment and management of glaucoma. Specifically, because of its poor lipoidal solubility, pilocarpine cannot rapidly penetrate the ophthalmic membrane, and as a consequence thereof, massive ophthalmic dosing is required in order to enable an antiglaucoma effective amount of pilocarpine to penetrate the ophthalmic membrane.
It is therefore quite obvious that a need exists for improved forms of pilocarpine which because of their extremely lipophilic nature, will rapidly penetrate the ophthalmic membrane and achieve reduction in intraocular pressure without the need for massive dosing.